isoflurane
Trade name: forane
Approved
Dec 18, 1979
Isoflurane (1-chloro-2, 2,2-trifluoroethyl difluoromethyl ether) a nonflammable liquid administered by vaporizing, is a general inhalation anesthetic drug. Isoflurane is a clear, colorless, stable liquid containing no additives or chemical stabilizers. Similar to many general anesthetics, the exact mechanism of the action has not been clearly delineated. Isoflurane reduces pain sensitivity (analgesia) and relaxes muscles. Isoflurane likely potentiates GABA-A and glycine receptor activity, which decreases motor function, inhibits receptor activity in the NMDA glutamate receptor subtypes and binds to glutamate receptors. Isoflurane is always administered in conjunction with air and/or pure oxygen. Often nitrous oxide is also used. Although its physical properties imply that anesthesia can be induced more rapidly than with halothane, its pungency can irritate the respiratory system, negating this theoretical advantage conferred by its physical properties. It is usually used to maintain a state of general anesthesia that has been induced with another drug, such as thiopentone or propofol. — NCATS
Clinical trial activity
90 trials · 92 clinical orgs · 7 marketing orgs
Earliest trial started Apr 1, 1994 (NCT00000251)
Timeline
1970s
1990s
- Jan 25, 1993
Hospira — Marketing Organization
- Jan 1, 1994
Earliest Phase 2 Sponsor(trial)
- May 12, 1995
Watson Pharmaceuticals — Marketing Organization
- Jun 27, 1995
Piramal — Marketing Organization
- Oct 20, 1999
Halocarbon Products — Marketing Organization
2020s
- Nov 4, 2025
Shandong Lanjin Pharmaceuticals Co.,Ltd — Marketing Organization
Indications
Approved for
Studied for
- Airway Extubation · Phase 4
- Alzheimer Disease · Phase 4
- Anesthesia · Phase 4
- Anesthesia, General · Phase 4
- Anesthetics, Inhalation · Phase 3
- Aortic Valve Insufficiency · Phase 3
- Breast Neoplasms · Phase 4
- Cardiovascular Diseases · Phase 4
- Cognition Disorders · Phase 4
- Colorectal Neoplasms · Phase 4
- Coronary Artery Bypass · Phase 4
- Coronary Artery Disease · Phase 1
- Coronary Disease · Phase 4
- COVID-19 · Phase 3
- Delirium · Phase 4
- Depression · Phase 2
- Depressive Disorder, Treatment-Resistant · Phase 2
- DNA Damage · Phase 4
- Drug-Related Side Effects and Adverse Reactions · Phase 3
- General Surgery · Phase 4
- Health · Phase 4
- Healthy Volunteers · Phase 4
- Heart Diseases · Phase 1
- Hematoma, Subdural, Acute · Phase 4
- Hemodynamics · Phase 4
- Hernia, Inguinal · Phase 3
- Hydrocephalus · Phase 3
- Hypertension, Pulmonary · Phase 4
- Hypotension · Phase 4
- Intensive Care Units, Pediatric · Phase 3
- Intestinal Pseudo-Obstruction · Phase 4
- Kidney Diseases · Phase 3
- Kidney Transplantation · Phase 2
- Liver Transplantation · Phase 2/Phase 3
- Lung Diseases · Phase 3
- Lung Neoplasms · Phase 4
- Major Depressive Disorder · Phase 2
- Melanoma · Phase 4
- Mitral Valve Insufficiency · Phase 3
- Myocardial Reperfusion Injury · Phase 4
- Myocardium · Phase 2/Phase 3
- Nausea · Phase 4
- Neoplasms · Phase 4
- Opioid-Related Disorders · Phase 2
- Postoperative Complications · Phase 4
- Postoperative Pain · Phase 4
- Procedural Sedation · Phase 4
- Prostatic Neoplasms · Phase 4
- Renal Insufficiency · Phase 4
- Respiratory Distress Syndrome · Phase 2/Phase 3
- Shock, Septic · Phase 4
- Sleep · Phase 4
- Stroke · Phase 4
- Subarachnoid Hemorrhage · Phase 4
- Substance-Related Disorders · Phase 2
- Surgical Oncology · Phase 4
- Thoracic Surgery · Phase 4
- Tympanic Membrane Perforation · Early Phase 1
- Ventilation · Phase 3
- Ventilators, Mechanical · Phase 2/Phase 3
- Ventricular Dysfunction · Phase 4
- Vomiting · Phase 4
Mechanism of action
- GABA-A receptor; anion channelPOSITIVE ALLOSTERIC MODULATOR
GABA-A receptor; anion channel positive allosteric modulator
Likely allosteric but unclear whether benzodiazepine or barbiturate site involved
- Gamma-aminobutyric acid receptor subunit alpha-1 (GABRA1) ↗
- Gamma-aminobutyric acid receptor subunit beta-2 (GABRB2) ↗
- Gamma-aminobutyric acid receptor subunit gamma-2 (GABRG2) ↗
- Gamma-aminobutyric acid receptor subunit beta-3 (GABRB3) ↗
- Gamma-aminobutyric acid receptor subunit alpha-4 (GABRA4) ↗
- Gamma-aminobutyric acid receptor subunit gamma-3 (GABRG3) ↗
- Gamma-aminobutyric acid receptor subunit theta (GABRQ) ↗
- Gamma-aminobutyric acid receptor subunit alpha-3 (GABRA3) ↗
- Gamma-aminobutyric acid receptor subunit pi (GABRP) ↗
- Gamma-aminobutyric acid receptor subunit delta (GABRD) ↗
- Gamma-aminobutyric acid receptor subunit gamma-1 (GABRG1) ↗
- Gamma-aminobutyric acid receptor subunit beta-1 (GABRB1) ↗
- Gamma-aminobutyric acid receptor subunit epsilon (GABRE) ↗
- Gamma-aminobutyric acid receptor subunit alpha-2 (GABRA2) ↗
- Gamma-aminobutyric acid receptor subunit alpha-5 (GABRA5) ↗
- Gamma-aminobutyric acid receptor subunit alpha-6 (GABRA6) ↗
- GABA receptor alpha-1 subunit
- GABA receptor beta-2 subunit
- GABA receptor alpha-4 subunit
- GABA receptor delta subunit
- GABA receptor alpha-5 subunit
- GABA receptor alpha-6 subunit
- GABA receptor beta-3 subunit
- GABA receptor alpha-3 subunit
- GABA receptor alpha-2 subunit
- GABA-A receptor; GABA-A site (alpha1/beta2 interface)
- GABA-A receptor; alpha-3/beta-3/gamma-2
- GABA-A receptor; alpha-1/beta-3/gamma-2
- GABA-A receptor; alpha-5/beta-3/gamma-2
- GABA-A receptor; alpha-2/beta-3/gamma-2
- GABA-A receptor; alpha-1/beta-2/gamma-2
- GABA-A receptor; alpha-6/beta-3/gamma-2
- GABA-A receptor; benzodiazepine site
- GABA-A receptor; agonist GABA site
- GABA A receptor alpha-2/beta-2/gamma-2
- GABA A receptor alpha-3/beta-2/gamma-2
- GABA A receptor alpha-6/beta-2/gamma-2
- GABA A receptor alpha-1/beta-1/gamma-2
- GABA A receptor alpha-4/beta-3/gamma-2
- Gamma-aminobutyric acid receptor subunit alpha-4/beta3/delta
- Gamma-aminobutyric acid receptor subunit alpha-1/ beta-1
- Gamma-aminobutyric acid receptor subunit alpha-2/beta-2
- Gamma-aminobutyric acid receptor subunit alpha-3/ beta-2
- Gamma-aminobutyric acid receptor subunit alpha-3/ beta-3/gamma-3
- Gamma-aminobutyric acid receptor subunit alpha-3/beta-3
- Gamma-aminobutyric acid receptor subunit alpha-3/beta-3/theta
- Gamma-aminobutyric acid receptor subunit alpha-5/beta-2
- Gamma-aminobutyric acid receptor subunit alpha-5/beta-3/gamma-3
- Gamma-aminobutyric acid receptor subunit alpha-6/beta-3
- GABA-A receptor alpha-1/beta-3
- Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/delta
- Gamma-aminobutyric acid receptor subunit alpha-4/beta-2/delta
- Gamma-aminobutyric acid receptor subunit beta-1/beta-2
- Gamma-aminobutyric acid receptor subunit alpha-5/beta-3
- Gamma-aminobutyric acid receptor subunit alpha-2/beta-3
- Gamma-aminobutyric acid receptor subunit alpha-1/alpha-2/beta-2/gamma-2
- Gamma-aminobutyric acid receptor subunit alpha-1/gamma-2
- Gamma-aminobutyric acid receptor subunit alpha-4/beta-2/gamma-2
- Gamma-aminobutyric acid receptor subunit alpha-4/beta-1/delta
- Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2
- GABA receptor beta-1 subunit
- Gamma-aminobutyric acid receptor subunit alpha-2/beta-1/gamma-2
- Glycine receptor (alpha-1/beta)POSITIVE MODULATOR
Glycine receptor (alpha-1/beta) positive modulator
alpha1/beta is main adult form
KCNK9 opener
KCNK10 opener
KCNK18 opener
KCNK3 opener
KCNK2 opener
Approval history
- approvedPriority reviewDec 18, 1979
Chemistry & pharmacology
SMILES
FC(F)OC(Cl)C(F)(F)F- Mol. weight
- 184.492 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- Yes
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
- Delivery
- Topical
- Availability
- Prescription Only
Oral
No
Parenteral
No
Topical
Yes
Sources
- WikipediaIsoflurane ↗
- NCATSCYS9AKD70P ↗
- ChEMBLCHEMBL1256 ↗
Also known as
- 1-chloro-2,2,2-trifluoroethyl difluoromethyl ether
- 1-chloro-2,2,2-trifluoroethyl difluoromethyl ether
- 1-chloro-2,2,2-trifluoroethyl difluoromethyl ether
- aerrane
- aerrane
- compound 469
- compound 469
- forane
- forane
- forane
- forane
- forene
- isoflurane
- isoflurane
- isoflurane
- isoflurane
- isoflurane
- isoflurane
- isoflurane
- isoflurane
- isoflurane
- isoflurane
- isoflurano
- isoflurano
- isofluranum
- isofluranum
- isoforine
- isorrane
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07099014 | Phase 3 | Sep 15, 2025 | Assistance Publique - Hôpitaux de Paris |
| NCT07152912 | N/A | Sep 4, 2025 | Ain Shams University |
| NCT07000526 | Phase 4 | Jul 31, 2025 | Universidad Autonoma de Madrid, Universidad Carlos III Madrid |
| NCT06252207 | N/A | Jan 15, 2025 | The Cleveland Clinic |
| NCT06624592 | Phase 3 | Nov 1, 2024 | Mayo Clinic |
| NCT06625606 | N/A | Sep 1, 2024 | Benha University |
| NCT06311604 | N/A | Jun 20, 2024 | University of Grenoble |
| NCT06387836 | N/A | Apr 23, 2024 | Fudan University |
| NCT05867472 | Phase 3 | Oct 10, 2023 | Canadian Institutes of Health Research (CIHR), University of Toronto |
| NCT06014138 | Phase 2/Phase 3 (Phase 3) | Sep 30, 2023 | Sedana Medical, University of London |
| NCT05993039 | Early Phase 1 (Phase 1) | Sep 1, 2023 | Louisiana State University, Our Lady of the Lake Regional Medical Center |
| NCT06418893 | Phase 2/Phase 3 (Phase 3) | Aug 1, 2023 | Institute of Liver and Biliary Sciences, India |
| NCT05639686 | N/A | Dec 1, 2022 | Louisiana State University, Our Lady of the Lake Regional Medical Center |
| NCT05327296 | Phase 3 | Jun 30, 2022 | Columbia University, Sedana Medical |
| NCT05312385 | Phase 3 | Apr 28, 2022 | Sedana Medical, Vanderbilt University |
| NCT06809218 | Phase 3 | Apr 22, 2022 | Sedana Medical, University of California, San Francisco |
| NCT05314569 | Phase 1 | Apr 15, 2022 | Cairo University |
| NCT05693428 | N/A | Jan 22, 2022 | Astana Medical University |
| NCT05742789 | Phase 1 | Nov 30, 2021 | Astana Medical University |
| NCT05695287 | Phase 1 | Jan 22, 2021 | Astana Medical University |
Organizations
Research & Development (92)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Sedana Medical | Academic/Hospital | 5 | 4 | 1 | 2020 |
| University of Toronto | Academic/Hospital | 5 | 5 | 2 | 2009 |
| Astana Medical University | Academic/Hospital | 4 | 4 | 3 | 2020 |
| Duke University | Academic/Hospital | 4 | 4 | 3 | 2006 |
| Fundação de Amparo à Pesquisa do Estado de São Paulo | Academic/Hospital | 3 | 0 | 2 | 2008 |
| Vanderbilt University | Academic/Hospital | 3 | 2 | 2 | 2016 |
| Ain Shams University | Academic/Hospital | 2 | 2 | 1 | 2021 |
| Cairo University | Academic/Hospital | 2 | 2 | 2 | 2020 |
| Columbia University | Academic/Hospital | 2 | 1 | 2 | 2003 |
| Louisiana State University | Academic/Hospital | 2 | 0 | 2 | 2022 |
| Mansoura University | Academic/Hospital | 2 | 2 | 1 | 2016 |
| Nanjing Medical University | Academic/Hospital | 2 | 2 | 2 | 2007 |
| National Institute on Drug Abuse (NIDA) | Government | 2 | 0 | 1 | 1994 |
| Ohio State University | Academic/Hospital | 2 | 2 | 1 | 2015 |
| Our Lady of the Lake Regional Medical Center | Academic/Hospital | 2 | 2 | 2 | 2022 |
| Ruhr University Bochum | Academic/Hospital | 2 | 2 | 1 | 2014 |
| RWTH Aachen University | Academic/Hospital | 2 | 1 | 2 | 2012 |
| Sao Paulo State University | Academic/Hospital | 2 | 2 | 1 | 2008 |
| University of Bern | Academic/Hospital | 2 | 2 | 1 | 2004 |
| University of Chicago | Academic/Hospital | 2 | 2 | 1 | 1994 |
Marketing (9)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Baxalta | For profit | NDA | Dec 18, 1979 |
| Baxter | For profit | NDA2 | Dec 18, 1979 |
| Halocarbon Products | For profit | MKTG | Oct 20, 1999 |
| Hospira | For profit | MKTG | Jan 25, 1993 |
| Piramal | For profit | MKTG | Jun 27, 1995 |
| Piramal | For profit | SYN | Sep 30, 1994 |
| Piramal | For profit | MKTG | Jun 27, 1995 |
| Shandong Lanjin Pharmaceuticals Co.,Ltd | For profit | MKTG | Nov 4, 2025 |
| Watson Pharmaceuticals | For profit | MKTG | May 12, 1995 |